Back to results
US 2007/0167381 A1Published application
Macrolides with antiinflammatory activity
AssigneeZambon Group S.p.A.
InventorsAndrea Mereu, Mauro Napoletano, Fernando Ornaghi, Ermanno Moriggi, Franco Pellacini
Life of this patent
Estimating the term…
Abstract
Macrolide compounds of formula (I) wherein X, R, R1, R2, R3 and R4, have the meanings as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and the use thereof in the treatment and prophylaxis of inflammatory diseases, are described.
Claims18
1) A compound of formula
- wherein
- X is a —C(═O)—, —C(═O)—O—, —C(═O)—N—, —SO2— or —SO2—N group;
- R is a hydrogen atom or methyl;
- R1 is a hydrogen atom or a (C1-C3)-alkyl group;
- R2 is a hydrogen atom, a (C1-C4)-alkoxy-(C1-C4)-alkyl group, a (C5-C7)-cycloalkyl group, a phenyl or a five- or six-membered heteroaryl having from one to three heteroatoms selected among nitrogen, oxygen and sulphur, a phenyl-(C1-C4)-alkyl or heteroaryl-(C1-C4)-alkyl group optionally substituted by 1 to 3 substituents selected among a (C1-C4)-alkyl group, a (C1-C4)-alkoxy group and halogen, or a chain of formula
- —(CH2)r—Y—(CH2)m-A
- wherein
- A is a phenyl or a five- or six-membered heteroaryl having from one to three heteroatoms selected among nitrogen, oxygen and sulphur, both ones optionally substituted by 1 to 3 substituents selected among a (C1-C4)-alkyl group, a (C1-C4)-alkoxy group or halogen;
- Y represents O, S or NR6 wherein R6 is a hydrogen atom, a linear or branched (C1-C3) alkyl, a (C1-C3)-alkoxycarbonyl group or a benzyloxycarbonyl group;
- r is an integer comprised between 1 and 3;
- m is an integer comprised between 0 and 3;
- R3 is a hydroxy group or R3 taken together with R4 forms a (═O) group or a ═N—O—R5 group wherein R5 is a hydrogen atom, a (C1-C4)-alkyl group, a benzyl or a —X—R2 group wherein X and R2 have the corresponding meanings defined above;
- R4 is a hydrogen atom or R4 taken together with R3 forms a (═O) group or a ═N—O—R5 group wherein R5 has the meanings defined above;
- and furthermore R2 is a (C1-C10)-alkyl group or a (C4-C10)-alkyl group when, at the same time, X is a —C(═O)— group, R1 is a (C1-C3)-alkyl group and R3 is a hydroxy group or R3 taken together with R4 forms a ═N—O—R5 group wherein R5 is different from —X—R2;
- and pharmaceutically acceptable salts thereof.
12 more elements
Dependencies are inferred from the claim text.